Exam 2

Question 1

if a drug is formulated in a solution, suspension, and a tablet, which would have the best chemical stability?

Answer 1

tablet, less degradation of drug so least reactive

Question 2

optimize the absorption rate of drug, increase the ease of administration by the patient, control the rate and site of drug absorption, mask the taste of therapeutic agent, improve chemical stability of drug

Answer 2

solid dosage forms designed to do all these things

Question 3

increased stability (solid dosage forms have longest shelf life), ease of packaging/storage/dispensing, convenience and accurate dosing, little to no taste/smell of drug

Answer 3

advantages of solid dosage forms

Question 4

solubility (drug must dissolve from solid dosage form), not suitable for some patients (pediatric/geriatric, patients have difficulty swallowing solid dosage forms - dysphagia), solid dosage forms not suitable for some routes of administration (IV, transdermal, ophthalmic, otic), some drugs lose their activity in solid form (therapeutic proteins, several biological products)

Answer 4

limitations of solid dosage forms

Question 5

evaluate the impact of physiochemical characteristics of the drug (API) and excipients (solubility, dissolution rate, permeability, drug-excipient compatibility, stability), suitability and therapeutic activity of final drug product (quality, stability, marketability, patient acceptance, cost)

Answer 5

performulation studies

Question 6

drug particles in some solid products are often micronized, this process increases….

Answer 6

dissolution rate of the drug (decrease the particle size)

Question 7

purity (efficacy and safety), organoleptic properties (color, odor, taste), presence of polymorphs (crystal forms), surface properties (wettability), particle size and size distribution (monodisperse - uniform particle size vs polydisperse - different particle sizes)

Answer 7

solid-state properties

Question 8

which has faster dissolution rate, higher solubility, but lower stability?(amorphous or crystalline)

Answer 8

amorphous structures

Question 9

what is the function of a wetting agent in solid dosage forms?

Answer 9

increase contact between drug particles and liquid

Question 10

what is used to measure the wetting of a substance by a liquid?

Answer 10

contact angle, lower angle number greater contact

Question 11

a hygroscopic drug is one that…

Answer 11

adsorbs moisture from the environment

Question 12

will take in moisture from the air until it gets saturated, want a drug that will not be this at low relative humidity, also need to take into consideration the amount of water being taken up (% weight change)

Answer 12

hygroscopicity

Question 13

stability issues, physical changes, dosing accuracy, microbial growth, packaging challenges

Answer 13

problems due to hygroscopicity

Question 14

methods to prevent problems due to hygroscopicity

Answer 14

moisture-resistant excipients, incorporate desiccants or moisture barriers, appropriate packaging materials, implement appropriate storage and handling practice

Question 15

particles are measured in ___________ but this can be a challenge with irregular particles, use __________

Answer 15

diameter, equivalent sphere

Question 16

examples of physical stability problems

Answer 16

capsules stick to each other, solvent from a solution evaporates, tablet dissolves slower than its specifications

Question 17

excipients for solid dosage forms

Answer 17

diluents, binders, disintegrants, lubricants, glidants, opacifiers

Question 18

a diluent is added to solid dosage formulations to…

Answer 18

act as a filler

Question 19

glidants/lubricants are added in the manufacture of solid dosage forms to…..

Answer 19

reduce friction among particles

Question 20

some excipients can perform more than one function, pre-processed and co-processed excipients, provide multiple functionalities to the formulation

Answer 20

multifunctional excipients

Question 21

mannitol-calcium silicate co-processed excipient

Answer 21

chewable properties, flowability, compressibility

Question 22

simple and convenient to use (solid unit dosage form), quick and safely manufactured into convenient doses for dose accuracy, carried in portable packages (improving compliance), can disguise unpleasant tastes with film coating, easily identified by markings, shape, and color for safety

Answer 22

tablet features

Question 23

not all drugs suitable for oral use, some drugs deactivated by the liver (first pass metabolism), may not be suitable for emergencies (slow onset of action, need for patient cooperation), not suitable for patients that can’t swallow, some drugs poorly absorbed by GI tract, pill-cheeking

Answer 23

drawbacks to tablets

Question 24

may affect drug product performance, makes powder blend more compact and affects tablet hardness

Answer 24

compression

Question 25

disintegrate slowly, results in slower rate of dissolution, reduces rate of systemic drug absorption, affecting the clinical response

Answer 25

excessive compression may cause tablets to do these things

Question 26

segregation of drugs from excipients (different particle sizes, density), friction between particles and between particles and equipment (clumping, sticking to equipment, poor flow)

Answer 26

problems with powders

Question 27

dust reduction (reduces fine particles), improved flowability (spherical shape, less contact surface), particle size and uniformity control (monodispersity), compaction enhancement (binders), improve dissolution profiles (hydrophilic excipients), increased bulk density (compact, dense)

Answer 27

reasons for granulation

Question 28

spraying, moistening, solidifying, finished agglomerate, HPC, MCC, PVP, starch, gelatin, sucrose, polyethylene glycol, drying with hot air

Answer 28

wet granulation

Question 29

to determine whether tablets or capsules disintegrate within the prescribed time, quality-assurance measure, USP sets standards for this

Answer 29

disintegration test

Question 30

control the rate and duration of drug release, target drug release to certain regions of the GI tract (small intestine or colon), plasticizers are added to render the coating flexible

Answer 30

film-coating tablets

Question 31

mask taste, odor, color of drugs/excipients, provide a smooth finish for easy swallowing, make the tablet physically stronger, protect from moisture, oxygen, light, protect form toxicity due to contact with drug, provide identification, brand recognition, facilitate printing, enable controlled/delayed release

Answer 31

reasons for coating tablets

Question 32

orange peel effect (roughness), blistering and film cracking, sticking (tablets stick together), bridging (coating bridges across logo), chipping (edge of tablet chips), color variation, tablet breakage, most of these are manufacturing issues but bad storage conditions can lead to these

Answer 32

tablet coating defects

Question 33

required strength unavailable, fractional doses in flexible, increasing, decreasing dosage regimen (dose titration, as needed dosing), ease of swallowing, cost

Answer 33

why tablet split

Question 34

dose uniformity (does the tablet split exactly into two equal parts?), do not crush list (is it proper to split a tablet not scored by the manufacturer?), how much of the tablet crumbles into fragments?, how easy is the process of splitting for elderly or disabled patients?

Answer 34

tablet splitting

Question 35

crumbling, uneven sizes, waste, lack of dexterity, confusion about dose, forgetting to split

Answer 35

concerns with splitting scored tablets

Question 36

dose dumping of controlled release products, destroy enteric coating, poorer stability, bitter taste, unwanted increase in dissolution rate, danger of exposure to the drug, patient's counseling

Answer 36

dangers of splitting unscored tablets

Question 37

coated with a polymer that does not dissolve under acidic conditions (stomach) but does dissolve under the more alkaline conditions of the small intestine (pH greater than 4), protection against possible drug degradation, reducing or preventing irritation of gastric mucosa

Answer 37

enteric coated tablets

Question 38

separation of drugs into separate layers that may be incompatible when formulated as a single layer, conventional tablet, delivery of therapeutic agents at different rates or to different sites within GI tract

Answer 38

multilayer tablets

Question 39

reaction between weak acid and bicarbonate produces carbon dioxide, helps mask taste, provide faster dissolution, allow administration of a large dose

Answer 39

effervescent tablets

Question 40

tablets are chewed before swallowing, suitable for patients who have difficulty swallowing conventional tablets (pediatric, some adults), large size tablets (antacid formulations)

Answer 40

chewable tablets

Question 41

rapid disintegration in the mouth, no need for water, improve adherence, 3D printed tabs, lyophilized (freeze dried tablets), loosely compressed, molded tablets

Answer 41

orally disintegrating tablets (ODT)

Question 42

tablets administered under the tongue, small and flat tablet, suitable for conditions like angina, or migraine

Answer 42

sublingual tablets

Question 43

tablet or film in the cheek or upper gum

Answer 43

buccal

Question 44

patient measures out individual doses, limited to relatively non-potent drugs like laxatives, antacids, dietary supplements

Answer 44

bulk powders/granules

Question 45

single doses in individual containers

Answer 45

divided powders/granules

Question 46

1. patients who cannot swallow 2. longer shelf-life (more stable) 3. convenient for dispensing drugs with a high dose 4. medicaments have faster dissolution rate than tablets/capsules (drug release from powders/granules will be faster than from the corresponding tablets/capsules 5. easy to formulate (compounding)

Answer 46

why powders/granules as dosage forms

Question 47

less convenient for the patient to carry/administer, masking of unpleasant tastes may be problematic, bulk powders/granules not suitable for administration of potent drugs, not suitable for drugs that are inactivated in stomach, cause damage to stomach, sustained or controlled drug delivery

Answer 47

limitations of powders/granules

Question 48

the particle size distribution of a powder is determined by.....

Answer 48

analytical sieving (USP)

Question 49

to prevent segregation of ingredients in powder mix for dose uniformity, improve flow properties of mix (ease of dosing, reduce the loss of drug in packaging), improve compaction characteristics of mix (packaging), reduce dust (easier handling)

Answer 49

reasons for granulation

Question 50

protects against light, air, moisture (improve chemical stability of API), multi-compositions (various release profiles like immediate and sustained release beads, chemically incompatible drugs physically separated), good flowability, mask taste and smell

Answer 50

benefits of particle coating

Question 51

diluent/filler, glidant, lubricant, coloring and flavoring agents

Answer 51

excipients in powders/granules

Question 52

solid dosage forms in which the API and excipients are enclosed within a soluble container/shell, shell may be composed of body and cap or single piece, shells usually made from gelatin but can be made from vegetable products, most designed for oral administration

Answer 52

capsules USP definition

Question 53

hard shell (powder/powder-like contents), soft shell (oils/oily semisolid formulations), modified-release (delayed or extended release)

Answer 53

types of capsules

Question 54

dipping, spinning, drying, stripping, trimming/cutting, joining

Answer 54

steps in production of hard gelatin capsule shells

Question 55

1. gelatin: type A and B gelatin 2. water: 12-16%, functions as plasticizer (additional plasticizers can be added if needed) 3. colorants, opacifying agents, wetting agents, and preservatives if needed

Answer 55

composition of empty hard gelatin capsule shells

Question 56

what will hygroscopic materials do to capsule shells?

Answer 56

may dry out the capsule shell and cause it to become brittle

Question 57

what will efflorescent materials do to capsule shells?

Answer 57

soften the capsules (take up water)

Question 58

1. rectification: placing empty gelatin capsules with bodies facing downward 2. separation: of caps from bodies 3. dosing: of fill material, the body is filled with formulation, dosing-disc machine/dosator machine 4. replacement of caps: and closing capsule shells 5. ejection: of filled capsules

Answer 58

capsule filling basic steps

Question 59

spraying, warming, setting

Answer 59

fusion-sealing process of capsule sealing which prevents leaks and is tamper-proof/evident

Question 60

oral softgels, chewable softgels, enteric softgels

Answer 60

types of soft gelatin capsules

Question 61

test to measure the strength of a gel/gelatin, determines the weight in grams needed by a specified plunger to depress the surface of the gel 4 mm without breaking it at a specified temperature

Answer 61

bloom strength

Question 62

high bloom strength gelatin is used in manufacturing of.....

Answer 62

hard shell capsules

Question 63

shells of soft gelatin capsules may be made elastic/plastic by the addition of....

Answer 63

sorbitol (plasticizer)

Question 64

1. gelatin 2. water (4-10%) 3. plasticizer 4. preservatives 5. coloring and opacifying agents 6. flavorings and sweeteners

Answer 64

composition of soft gelatin capsule shells

Question 65

hygroscopic, volatile, acidic, aldehyde materials

Answer 65

can't use these in filling softgels